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PT2977 (Belzutifan) HIF-2α inhibitor

Name: PT2977 (Belzutifan)
Brand: Selleck Chemicals
SKU: S8886
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S8886

Belzutifan (PT2977), an orally active and selective HIF-2α inhibitor, increases potency and improves pharmacokinetic profile, providing a potential treatment for clear cell renal cell carcinoma (ccRCC).

Chemical Structure

Molecular Weight: 383.34

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Quality Control

Batch: S888601 DMSO]77 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.79%

Cited in Nature Medicine for its top-tier quality
COA
SDS/MSDS
Datasheet

99.79

Related Targets	HSP JNK Antioxidant ROS eIF IRE1 PERK PDI PKR ASK
Other HIF Inhibitors	PT2399 PX-478 Dihydrochloride BAY 87-2243 KC7F2 IOX2 Molidustat (BAY 85-3934) CAY10585 (LW 6) PT2385 IDF-11774 FG-2216

Solubility in DMSO or Water

In vitro
Batch:

DMSO : 77 mg/mL (200.86 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.850mg/ml (10.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 77 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (3.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Working Concentrations for Cell Culture Treatment

Working Concentrations for Animal Model Treatment

Mechanism of Action

Information	PT2977 (Belzutifan) is a potent HIF-2α inhibitor. It affects hypoxia signaling by binding to the HIF-2α PAS-B domain to disrupt HIF-2α/HIF-1β heterodimerization, effectively inhibiting hypoxia transcriptional programs, endothelial dysfunction, and tumor proliferation.
Read more about PT2977 (Belzutifan) IC50 for cell-based and cell-free assays
Primary Applications and Mechanism of Action

Chemical Information, Storage & Stability

Molecular Weight	383.34	Formula	C₁₇H₁₂F₃NO₄S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1672668-24-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	MK-6482			Smiles	CS(=O)(=O)C1=C2C(C(C(C2=C(C=C1)OC3=CC(=CC(=C3)C#N)F)F)F)O

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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